Abstract
BackgroundAlthough the pharmacological activities of the seed extract of Descurainia sophia have been proven to be useful against cough, asthma, and edema, the biologically active components, particularly at the molecular level, remain elusive. Therefore, we aimed to identify the active component of an ethanol extract of D. sophia seeds (EEDS) by applying a systematic genomic approach.ResultsAfter treatment with EEDS, the dose-dependently expressed genes in A549 cells were used to query the Connectivity map to determine which small molecules could closely mimic EEDS in terms of whole gene expression. Gene ontology and pathway analyses were also performed to identify the functional involvement of the drug responsive genes. In addition, interaction network and enrichment map assays were implemented to measure the functional network structure of the drug-responsive genes. A Connectivity map analysis of differentially expressed genes resulted in the discovery of helveticoside as a candidate drug that induces a similar gene expression pattern to EEDS. We identified the presence of helveticoside in EEDS and determined that helveticoside was responsible for the dose-dependent gene expression induced by EEDS. Gene ontology and pathway analyses revealed that the metabolism and signaling processes in A549 cells were reciprocally regulated by helveticoside and inter-connected as functional modules. Additionally, in an ontological network analysis, diverse cancer type-related genes were found to be associated with the biological functions regulated by helveticoside.ConclusionsUsing bioinformatic analyses, we confirmed that helveticoside is a biologically active component of EEDS that induces reciprocal regulation of metabolism and signaling processes. Our approach may provide novel insights to the herbal research field for identifying biologically active components from extracts.Electronic supplementary materialThe online version of this article (doi:10.1186/s12864-015-1918-1) contains supplementary material, which is available to authorized users.
Highlights
The pharmacological activities of the seed extract of Descurainia sophia have been proven to be useful against cough, asthma, and edema, the biologically active components, at the molecular level, remain elusive
The list of genes used for the Connectivity map analysis is shown in Additional file 1 for extract of D. sophia seeds (EEDS) and Additional file 2 for helveticoside
Connectivity map for the effect of EEDS on A549 human lung cancer cells We previously observed that EEDS treatment induced two major patterns of gene expression in A549 human lung cancer cells [6]
Summary
The pharmacological activities of the seed extract of Descurainia sophia have been proven to be useful against cough, asthma, and edema, the biologically active components, at the molecular level, remain elusive. We aimed to identify the active component of an ethanol extract of D. sophia seeds (EEDS) by applying a systematic genomic approach. The seeds of D. sophia have been used to treat various ailments, including cough, asthma, and edema. We previously isolated diverse compounds showing cytotoxic and anti-inflammatory activities, including glycosides, from the seeds of D. sophia [1]. Despite the therapeutic constituents that have been identified far in EEDS, the pharmacological effects of EEDS have not been wellcharacterized, on the molecular level, largely due to the chemical complexity of EEDS
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